Identification of drugs inhibiting the in vitro metabolism of tacrolimus by human liver microsomes

British Journal of Clinical Pharmacology

Volumn 41, Issue 3, 1996, Pages 187-190

  Christians, Uwe ^a   Schmidt, Gudrun ^a   Bader, Augustinus ^a   Lampen, Alfons ^a   Schottmann, Renate ^a   Linck, Annette ^a   Sewing, Karl Friedrich ^a  

^a HANNOVER MEDICAL SCHOOL   (Germany)

Author keywords

13 O demethyl tacrolimus; Cytochrome P450 3A; Drug interactions; Human microsomes; Metabolism; Tacrolimus

Indexed keywords

BROMOCRIPTINE; CORTICOSTERONE; CYTOCHROME P450; DEXAMETHASONE; ERGOTAMINE; ERYTHROMYCIN; ETHINYLESTRADIOL; JOSAMYCIN; KETOCONAZOLE; MICONAZOLE; MIDAZOLAM; NIFEDIPINE; OMEPRAZOLE; TACROLIMUS; TAMOXIFEN; TROLEANDOMYCIN; VERAPAMIL;

ARTICLE; DRUG ANTAGONISM; DRUG IDENTIFICATION; DRUG METABOLISM; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; HUMAN CELL; IN VITRO STUDY; LIVER MICROSOME; MICHAELIS MENTEN KINETICS; PRIORITY JOURNAL;

EID: 0029922323     PISSN: 03065251     EISSN: None     Source Type: Journal    
DOI: 10.1111/j.1365-2125.1996.tb00181.x     Document Type: Article

References (10)

1. Peters DH, Fitton A, Plosker GL, et al. Tacrolimus. A review of its pharmacology, and therapeutic potential in hepatic and renal transplantation. Drugs 1993; 46: 746-794.
2. Sattler M, Guengerich FP, Yun CH, et al. Cytochrome P-450 3A enzymes are responsible for biotransformation of FK506 and rapamycin in man and rat. Drug Metab Dispos 1992; 20: 753-761.
3. Iwasaki K, Shiraga T, Nagase K, et al. Isolation, identification and biological activities of oxidative metabolites of FK506, a potent immunosuppressive macrolide lactone. Drug Metab Dispos 1993; 21: 971-977.
4. Iwasaki K, Shiraga T, Matsuda K, et al. Further metabolism of FK506 (tacrolimus). Identification and biological activities of the metabolites oxidized at multiple sites of FK506. Drug Metab Dispos 1995; 23: 28-34.
5. Schüler W, Christians U, Schmieder P, et al. Structural identification of 13-demethyl-FK506 and its isomers generated by in-vitro metabolism of FK506 using human liver microsomes. Helv Chim Acta 1993; 76: 2288-2302.
6. Pichard L, Fabre I, Fabre G, et al. Cyclosporin A drug interactions. Screening for inducers and inhibitors of cytochrome P-450 (cyclosporin A oxidase) in primary cultures of human hepatocytes and liver microsomes. Drug Metab Dispos 1990; 18: 595-606.
7. Christians U, Kruse C, Kownatzki R, et al. Measurement of FK506 by HPLC and isolation and characterization of its metabolites. Transplant Proc 1991; 23: 940-941.
8. Gonschior AK, Christians U, Braun F, et al. Measurement of blood concentrations of FK506 (tacrolimus) and its metabolites in seven liver graft recipients after the first oral dose by HPLC-MS and microparticle enzyme immunoassay. Br J Clin Pharmacol 1994; 38: 567-571.
9. Shiraga T, Matsuda M, Nagase K, et al. Metabolism of FK506, a potent immunosupressive agent, by cytochrome P450 3A enzymes in rat, dog and human liver microsomes. Biochem Pharmacol 1993; 47: 727-735.
10. Karanam BV, Vincent SH, Lee Chiu SH. FK506 metabolism in human liver microsomes: Investigations of the involvement of cytochrome P450 isozymes other than CYP3A4. Drug Metab Dispos 1994; 22: 811-814.